CN1130342C - β－丙内酰胺的合成方法 - Google Patents

β－丙内酰胺的合成方法 Download PDF

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Publication number
CN1130342C
CN1130342C CN99814140A CN99814140A CN1130342C CN 1130342 C CN1130342 C CN 1130342C CN 99814140 A CN99814140 A CN 99814140A CN 99814140 A CN99814140 A CN 99814140A CN 1130342 C CN1130342 C CN 1130342C
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CN
China
Prior art keywords
formula
silyl
compound
protecting group
amino
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
CN99814140A
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English (en)
Chinese (zh)
Other versions
CN1329592A (zh
Inventor
T·K·蒂鲁文加达姆
X·付
C·－H·谭
T·L·麦阿利斯特
J·S·丘
C·科隆
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
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Schering Corp
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Application filed by Schering Corp filed Critical Schering Corp
Publication of CN1329592A publication Critical patent/CN1329592A/zh
Application granted granted Critical
Publication of CN1130342C publication Critical patent/CN1130342C/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C07F7/1872—Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892—Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN99814140A 1998-12-07 1999-12-06 β－丙内酰胺的合成方法 Expired - Lifetime CN1130342C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US20693198A 1998-12-07 1998-12-07
US09/206,931 1998-12-07

Publications (2)

Publication Number Publication Date
CN1329592A CN1329592A (zh) 2002-01-02
CN1130342C true CN1130342C (zh) 2003-12-10

Family

ID=22768573

Family Applications (1)

Application Number Title Priority Date Filing Date
CN99814140A Expired - Lifetime CN1130342C (zh) 1998-12-07 1999-12-06 β－丙内酰胺的合成方法

Country Status (13)

Country Link
EP (1) EP1137634B1 (enExample)
JP (3) JP3640888B2 (enExample)
CN (1) CN1130342C (enExample)
AR (1) AR025144A1 (enExample)
AT (1) ATE297892T1 (enExample)
AU (1) AU2030100A (enExample)
CA (1) CA2353981C (enExample)
DE (1) DE69925862T2 (enExample)
ES (1) ES2244238T3 (enExample)
HK (1) HK1039487B (enExample)
PT (1) PT1137634E (enExample)
WO (1) WO2000034240A1 (enExample)
ZA (1) ZA200104004B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101384532B (zh) * 2006-02-16 2013-01-02 寿制药株式会社 制造光学活性醇的方法

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AU2002247019C1 (en) 2001-01-26 2017-05-11 Organon Llc Combinations of peroxisome proliferator-activated receptor (PPAR) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
RU2756946C2 (ru) 2001-01-26 2021-10-07 Мерк Шарп И Доум Корп. Применение замещенных азетидинонов для лечения ситостеролемии
PL205952B1 (pl) 2001-03-28 2010-06-30 Schering Corp Sposób wytwarzania związków oksazolidynonowych
DE60216300T2 (de) 2001-09-21 2007-06-28 Schering Corp. Behandlung von xanthom mittels azetidinon-derivate als hemmer der sterol absorption
US7053080B2 (en) 2001-09-21 2006-05-30 Schering Corporation Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors
US7056906B2 (en) 2001-09-21 2006-06-06 Schering Corporation Combinations of hormone replacement therapy composition(s) and sterol absorption inhibitor(s) and treatments for vascular conditions in post-menopausal women
AU2003237593A1 (en) * 2002-06-05 2003-12-22 Natco Pharma Limited Process for the preparation of 4-(4-fluorobenzoyl) butyric acid
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US7135556B2 (en) 2002-07-19 2006-11-14 Schering Corporation NPC1L1 (NPC3) and methods of use thereof
CA2504878A1 (en) 2002-11-06 2004-05-27 Schering Corporation Cholesterol absorption inhibitors for the treatment of demyelination
MXPA05009501A (es) 2003-03-07 2005-10-18 Schering Corp Compuestos de azetidinona sustituidos, formulaciones y usos de los mismos para el tratamiento de hipercolesterolemia.
EP1601668B1 (en) 2003-03-07 2008-08-27 Schering Corporation Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia
MXPA05009502A (es) 2003-03-07 2005-10-18 Schering Corp Compuestos de azetidinona sustituidos, formulaciones y usos de los mismos para el tratamiento de hipercolesterolemia.
US7459442B2 (en) 2003-03-07 2008-12-02 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
AR041089A1 (es) 2003-05-15 2005-05-04 Merck & Co Inc Procedimiento y composiciones farmaceutiicas para tratar aterosclerosis, dislipidemias y afecciones relacionadas
EP1687287A1 (en) 2003-11-24 2006-08-09 Hetero Drugs Limited A novel process for ezetimibe intermediate
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US20060211752A1 (en) 2004-03-16 2006-09-21 Kohn Leonard D Use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune/inflammatory diseases associated with toll-like receptor overexpression
WO2006050634A1 (en) * 2004-11-15 2006-05-18 Xiamen Mchem Pharma (Group) Ltd. A preparation method of 1-(4-fluorophenyl)-(3r)-[3-(4-fluorophenyl)-(3s)-hydroxypropyl]-(4s)-(4-hydroxyphenyl)-2-azetidinone
HRP20121007T1 (hr) * 2004-12-20 2013-01-31 Merck Sharp & Dohme Corp. Postupak za sintezu azetidinona
TW200726746A (en) * 2005-05-06 2007-07-16 Microbia Inc Processes for production of 4-biphenylylazetidin-2-ones
KR20080017345A (ko) * 2005-05-11 2008-02-26 마이크로비아 인코포레이티드 페놀성 4-비페닐일아제티딘-2-온의 제조방법
US20090099355A1 (en) * 2005-05-25 2009-04-16 Microbia, Inc. Processes for Production of 4-(Biphenylyl)Azetidin-2-One Phosphonic Acids
SA06270191B1 (ar) 2005-06-22 2010-03-29 استرازينيكا ايه بي مشتقات من 2- أزيتيدينون جديدة باعتبارها مثبطات لامتصاص الكوليسترول لعلاج حالات فرط نسبة الدهون في الدم
WO2007017705A1 (en) * 2005-08-09 2007-02-15 Glenmark Pharmaceuticals Limited Process for the preparation of azetidinones
US20080255084A1 (en) 2005-10-21 2008-10-16 Randy Lee Webb Combination of Organic Compounds
HU0501164D0 (en) * 2005-12-20 2006-02-28 Richter Gedeon Vegyeszet New industrial process for the production of ezetimibe
WO2007100807A2 (en) 2006-02-24 2007-09-07 Schering Corporation Npc1l1 orthologues
AR060623A1 (es) 2006-04-27 2008-07-02 Astrazeneca Ab Compuestos derivados de 2-azetidinona y un metodo de preparacion
CN100564357C (zh) * 2006-10-20 2009-12-02 浙江天宇药业有限公司 一种氮杂环丁酮衍生物及其合成方法
CZ305066B6 (cs) * 2008-02-25 2015-04-22 Zentiva, K.S. Způsob výroby (3R,4S)-1-(4-fluorfenyl)-3-[(3S)-3-(4-fluorfenyl)-3-hydroxypropyl)]-4-(4-hydroxyfenyl)-2-azetidinonu
AR074752A1 (es) * 2008-12-17 2011-02-09 Hanmi Pharm Ind Co Ltd Metodo para preparar ezetimiba e intermediarios usados en la misma
EP2414529A2 (en) 2009-04-01 2012-02-08 Matrix Laboratories Ltd Enzymatic process for the preparation of (s)-5-(4-fluoro-phenyl)-5-hydroxy- 1morpholin-4-yl-pentan-1-one, an intermediate of ezetimibe and further conversion to ezetimibe
WO2010141494A2 (en) * 2009-06-02 2010-12-09 Codexis, Inc. Synthesis of ezetimibe
CN101935309B (zh) * 2009-06-29 2013-11-13 上海特化医药科技有限公司 依泽替米贝的制备方法及其中间体
CN101845010B (zh) * 2010-02-10 2012-07-25 浙江大学 一种制备伊替米贝的方法
ES2372460B1 (es) 2010-07-09 2012-11-16 Moehs Ibérica S.L. Nuevo método para la preparación de ezetimiba.
WO2012076030A1 (en) * 2010-12-10 2012-06-14 Pharmathen S.A. Process for the preparation of intermediate compounds useful in the preparation of ezetimibe
CN103570574B (zh) 2012-07-20 2016-04-13 中国科学院上海有机化学研究所 一种依泽替米贝的合成方法及该方法中所用的中间体
CN103102297A (zh) * 2012-09-28 2013-05-15 北京赛林泰医药技术有限公司 一种新的依折麦布的合成方法
CN103864708A (zh) * 2012-12-12 2014-06-18 天津市医药集团技术发展有限公司 一种依折麦布中间体的制备方法
WO2015039675A1 (en) 2013-09-23 2015-03-26 Pharmathen S.A. Novel process for the preparation of ezetimibe intermediates
CN103739537B (zh) * 2013-12-24 2015-05-20 连云港恒运医药科技有限公司 依折麦布的新合成方法
CN103819382A (zh) * 2014-01-01 2014-05-28 北京万全德众医药生物技术有限公司 一种依折麦布杂质的制备方法
CN103965089B (zh) * 2014-04-18 2016-06-29 上海方楠生物科技有限公司 一种立体选择性的合成降血脂药物依折麦布的方法
CN104230978B (zh) * 2014-09-22 2016-09-28 上海现代制药股份有限公司 依折麦布的制备中间体及其制备方法
CN104447474A (zh) * 2014-11-11 2015-03-25 武汉武药科技有限公司 一种依折麦布异构体的合成方法
CN104402790B (zh) * 2014-12-28 2016-09-28 严白双 一种制备依折麦布的改进工艺
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CN104892537B (zh) * 2015-05-15 2018-07-17 江西施美药业股份有限公司 依折麦布中间体以及依折麦布的合成方法
CN104829511A (zh) * 2015-05-18 2015-08-12 广州南新制药有限公司 一种依折麦布的合成工艺
CN105237492A (zh) * 2015-10-29 2016-01-13 无锡福祈制药有限公司 一种依折麦布中间体的合成方法
CN105524010B (zh) * 2015-12-16 2018-10-26 江苏恒盛药业有限公司 一种依泽麦布中间体及其制备方法
CN105566243B (zh) * 2016-01-15 2017-10-31 齐鲁天和惠世制药有限公司 从依折麦布生产废液中回收(s)‑(+)‑4‑苯基‑2‑噁唑烷酮的方法
CN107098841A (zh) * 2016-02-19 2017-08-29 常州方楠医药技术有限公司 一种依折麦布的制备方法及该方法中所用的中间体
JP6711709B2 (ja) * 2016-05-10 2020-06-17 株式会社トクヤマ エゼチミブの製造方法
CN106967106B (zh) * 2017-04-24 2018-08-10 上海华源医药科技发展有限公司 一种依折麦布中间体的生产方法
JP6802121B2 (ja) 2017-08-04 2020-12-16 株式会社シマノ 自転車用コンポーネント
CN110818606B (zh) * 2018-08-08 2021-06-29 上海博志研新药物技术有限公司 依折麦布及其中间体的制备方法
CN112441959A (zh) * 2020-12-07 2021-03-05 石家庄市华新药业有限责任公司 一种依折麦布原料药合成工艺
CN115850144A (zh) * 2022-12-30 2023-03-28 湖南方盛绿色合成制药有限公司 依折麦布的制备工艺
CN116283948A (zh) * 2023-02-24 2023-06-23 江苏阿尔法药业股份有限公司 一种依折麦布中间体的合成方法
CN117843543A (zh) * 2024-01-02 2024-04-09 南京工业大学 一种α,α-二氟丁内酰胺的制备方法

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Also Published As

Publication number Publication date
DE69925862T2 (de) 2006-05-04
JP3640888B2 (ja) 2005-04-20
CA2353981A1 (en) 2000-06-15
AU2030100A (en) 2000-06-26
JP4616620B2 (ja) 2011-01-19
JP2002531546A (ja) 2002-09-24
EP1137634A1 (en) 2001-10-04
JP2011016841A (ja) 2011-01-27
ES2244238T3 (es) 2005-12-01
CN1329592A (zh) 2002-01-02
DE69925862D1 (de) 2005-07-21
HK1039487B (en) 2005-08-12
AR025144A1 (es) 2002-11-13
WO2000034240A1 (en) 2000-06-15
CA2353981C (en) 2005-04-26
PT1137634E (pt) 2005-10-31
HK1039487A1 (en) 2002-04-26
EP1137634B1 (en) 2005-06-15
ATE297892T1 (de) 2005-07-15
JP2005053931A (ja) 2005-03-03
ZA200104004B (en) 2002-08-16

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